(1) Field of the Invention
The invention relates to novel anthrasteroid derivatives represented by the following general formula (I) which are effective against androgen-dependent diseases especially against prostatic hypertrophy, prostatic cancer and so forth. ##STR2## wherein R is hydrogen or lower alkyl; X is hydrogen, lower alkyl, halogen, hydroxy, hydroxymethyl, or halomethyl; Y is C.dbd.O, CH.about.OR', or OH CR", wherein R' is hydrogen, lower alkyl, cycloalkyl which may have an unsaturated bond or a substituent, or aliphatic lower acyl which may have carboxy or its lower alkyl ester at the terminal; R" is lower alkyl or lower alkynyl; the dotted line indicates the presence or absence of double bond; and the wavy line indicates an .alpha. or .beta. configuration.
(2) Description of the Prior Art
In the treatment of androgen dependent-diseases, it is general to use a steroid hormone type medicine i.e. anti-androgen. As a well-known commercially available anti-androgen, cyproterone acetate, chlormadinone acetate, oxendolone or the like is exemplified.
As all of the above-mentioned commercially available antiandrogens have a normal steroid structure, the separation of antiandrogenicity from the native effects of steroid hormones is not sufficient. Occurrence of various side effects such as hypersensitiveness, gain of weight, gynecomastia, adrenal medullary insufficiency, feeling of fatigue, cephalalgia, feeling of lassitude, oligocythemia, pyrexia, loss of sexuality and so forth has been observed, accordingly.